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WO2011037896A3 - Modification de polypeptide - Google Patents

Modification de polypeptide Download PDF

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Publication number
WO2011037896A3
WO2011037896A3 PCT/US2010/049599 US2010049599W WO2011037896A3 WO 2011037896 A3 WO2011037896 A3 WO 2011037896A3 US 2010049599 W US2010049599 W US 2010049599W WO 2011037896 A3 WO2011037896 A3 WO 2011037896A3
Authority
WO
WIPO (PCT)
Prior art keywords
polypeptide
terminal cysteine
cysteine
thiol group
polypeptide modification
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Ceased
Application number
PCT/US2010/049599
Other languages
English (en)
Other versions
WO2011037896A2 (fr
WO2011037896A4 (fr
Inventor
Lee A. Henderson
G. Scott Fletcher
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Vybion Inc
Original Assignee
Vybion Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Vybion Inc filed Critical Vybion Inc
Priority to CA2775287A priority Critical patent/CA2775287A1/fr
Priority to EP10819315.2A priority patent/EP2480578A4/fr
Priority to US13/497,667 priority patent/US20120178914A1/en
Publication of WO2011037896A2 publication Critical patent/WO2011037896A2/fr
Publication of WO2011037896A3 publication Critical patent/WO2011037896A3/fr
Publication of WO2011037896A4 publication Critical patent/WO2011037896A4/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/56—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule
    • A61K47/59—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes
    • A61K47/60—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic macromolecular compound, e.g. an oligomeric, polymeric or dendrimeric molecule obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyureas or polyurethanes the organic macromolecular compound being a polyoxyalkylene oligomer, polymer or dendrimer, e.g. PEG, PPG, PEO or polyglycerol

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Analytical Chemistry (AREA)
  • Molecular Biology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Biophysics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Peptides Or Proteins (AREA)
  • Medicinal Preparation (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

La présente invention concerne des procédés de PEGylation d'une cystéine N-terminale d'un polypeptide de manière à ce que le groupe thiol de la cystéine n'ait pas réagi dans le polypeptide PEGylé. Dans un mode de réalisation, l'invention concerne un procédé de PEGylation d'un polypeptide ayant une cystéine N-terminale, le procédé comprenant : la mise en contact du polypeptide avec un dérivé de polyéthylène glycol (PEG) ayant un groupe aldéhyde libre dans le mélange réactionnel dans des conditions de réduction de manière à ce que la cystéine N-terminale sans le polypeptide PEGylé résultant ait un groupe thiol libre.
PCT/US2010/049599 2009-09-25 2010-09-21 Modification de polypeptide Ceased WO2011037896A2 (fr)

Priority Applications (3)

Application Number Priority Date Filing Date Title
CA2775287A CA2775287A1 (fr) 2009-09-25 2010-09-21 Modification de polypeptide
EP10819315.2A EP2480578A4 (fr) 2009-09-25 2010-09-21 Modification de polypeptide
US13/497,667 US20120178914A1 (en) 2009-09-25 2010-09-21 Polypeptide modification

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24577709P 2009-09-25 2009-09-25
US61/245,777 2009-09-25

Publications (3)

Publication Number Publication Date
WO2011037896A2 WO2011037896A2 (fr) 2011-03-31
WO2011037896A3 true WO2011037896A3 (fr) 2011-08-18
WO2011037896A4 WO2011037896A4 (fr) 2011-11-10

Family

ID=43796448

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/049599 Ceased WO2011037896A2 (fr) 2009-09-25 2010-09-21 Modification de polypeptide

Country Status (5)

Country Link
US (1) US20120178914A1 (fr)
EP (1) EP2480578A4 (fr)
CA (1) CA2775287A1 (fr)
TW (1) TW201117827A (fr)
WO (1) WO2011037896A2 (fr)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105838699A (zh) 2006-12-15 2016-08-10 巴克斯艾尔塔公司 具有延长的体内半衰期的因子VIIa-聚唾液酸结合物
EP2459226B1 (fr) 2009-07-27 2016-06-29 Lipoxen Technologies Limited Glyco-polysialylation de protéines autres que des protéines de coagulation du sang
US8642737B2 (en) 2010-07-26 2014-02-04 Baxter International Inc. Nucleophilic catalysts for oxime linkage
US8809501B2 (en) 2009-07-27 2014-08-19 Baxter International Inc. Nucleophilic catalysts for oxime linkage
PL2459224T3 (pl) 2009-07-27 2017-08-31 Baxalta GmbH Koniugaty białka związanego z krzepnięciem krwi
EP2459224B1 (fr) 2009-07-27 2016-06-01 Baxalta GmbH Conjugués de protéine de coagulation sanguine
ES2800983T3 (es) 2010-12-22 2021-01-07 Baxalta GmbH Materiales y métodos para conjugar un derivado de ácido graso soluble en agua con una proteína
EP2872166B1 (fr) 2012-07-16 2021-09-08 Yale University Compositions et méthodes permettant de détecter, traiter et prévenir des maladies et affections
US10046058B2 (en) 2014-12-02 2018-08-14 Rezolute, Inc. Use of hydrophobic organic acids to increase hydrophobicity of proteins and protein conjugates
AU2016270302B2 (en) 2015-06-04 2020-09-17 Rezolute, Inc. Amine pegylation methods for the preparation of site-specific protein conjugates

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5795569A (en) * 1994-03-31 1998-08-18 Amgen Inc. Mono-pegylated proteins that stimulate megakaryocyte growth and differentiation
US6608183B1 (en) * 1997-07-14 2003-08-19 Bolder Biotechnology, Inc. Derivatives of growth hormone and related proteins
US6753165B1 (en) * 1999-01-14 2004-06-22 Bolder Biotechnology, Inc. Methods for making proteins containing free cysteine residues
US20060210534A1 (en) * 2000-09-29 2006-09-21 Schering Corporation Pegylated interleukin-10
US20060233746A1 (en) * 1994-10-12 2006-10-19 Amgen Inc. N-terminally chemically modified protein compositions and methods

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007002233A2 (fr) * 2005-06-20 2007-01-04 Pepgen Corporation Analogues d'interferon-alpha humains a circulation longue et faible toxicite
CA2653717A1 (fr) 2006-05-26 2007-12-06 Societe De Conseils De Recherches Et D'applications Scientifiques S.A.S. Methodes de pegylation specifique d'un site

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5795569A (en) * 1994-03-31 1998-08-18 Amgen Inc. Mono-pegylated proteins that stimulate megakaryocyte growth and differentiation
US20060233746A1 (en) * 1994-10-12 2006-10-19 Amgen Inc. N-terminally chemically modified protein compositions and methods
US6608183B1 (en) * 1997-07-14 2003-08-19 Bolder Biotechnology, Inc. Derivatives of growth hormone and related proteins
US6753165B1 (en) * 1999-01-14 2004-06-22 Bolder Biotechnology, Inc. Methods for making proteins containing free cysteine residues
US20060210534A1 (en) * 2000-09-29 2006-09-21 Schering Corporation Pegylated interleukin-10

Also Published As

Publication number Publication date
US20120178914A1 (en) 2012-07-12
WO2011037896A2 (fr) 2011-03-31
EP2480578A2 (fr) 2012-08-01
EP2480578A4 (fr) 2013-04-17
CA2775287A1 (fr) 2011-03-31
WO2011037896A4 (fr) 2011-11-10
TW201117827A (en) 2011-06-01

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